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Original Paper
Pharmacology 2015;95:59–64
DOI: 10.1159/000370244
Antinociceptive Synergism of
Gabapentin and Nortriptyline in Mice
with Partial Sciatic Nerve Ligation
Hugo F. Miranda
a, b
Viviana Noriega
a, c
Ramiro Zepeda
b
Pilar Zanetta
b
Josefina Prieto-Rayo
d
Juan Carlos Prieto
b, c
Fernando Sierralta
e
a
School of Pharmacy, Faculty of Medicine, Universidad Andrés Bello,
b
Pharmacology Program, School of Medicine,
ICBM, Faculty of Medicine,
c
Cardiovascular Department, Clinic Hospital, and
d
Faculty of Dentistry, Universidad de
Chile, and
e
Dental School, Universidad Finis Terrae, Santiago, Chile
showed a synergy in antinociception at a gabapentin-to-
nortriptyline ratio of 1: 1 in PSNL mice. This finding suggests
that this combination could provide a therapeutic alterna-
tive that can be used for neuropathic pain management.
© 2015 S. Karger AG, Basel
Introduction
Neuropathic pain is a type of pain that is distinguish-
able from other types because it results from nerve dam-
age or dysfunction in either the peripheral or the central
nervous system. Neuropathic pain can be induced by au-
toimmune disease, metabolic diseases, infection, posther-
petic neuralgia, vascular disease, stroke, trauma, and can-
cer [1]. Distinct neurophysiological and neurochemical
mechanisms contribute to neuropathic pain. Tissue in-
jury can trigger the release of pronociceptive mediators
that induce a sensitization of the peripheral nerve termi-
nals. Modifications of the sensory neurons can also occur
Key Words
Neuropathic pain · Hot plate test · Hyperalgesia ·
Isobolographic analysis · Synergy
Abstract
Background and Methods: Neuropathic pain results from
nerve injury, and gabapentin, an antiepileptic drug, has
been approved for the treatment of several types of neuro-
pathic pain. On the other hand, nortriptyline, an antidepres-
sant drug, has been suggested as an alternative treatment.
In partial sciatic nerve ligation (PSNL) mice, the interaction of
gabapentin with nortriptyline was evaluated by the hot
plate assay using isobolographic analysis. Results: Gaba-
pentin (3–100 mg/kg, i.p.) or nortriptyline (1–30 mg/kg, i.p.)
induced dose-dependent antinociception, with an ED
50
of
11.60 ± 0.54 mg/kg for gabapentin and of 5.16 ± 0.21 mg/kg
for nortriptyline. The potency of gabapentin and nortripty-
line in PSNL mice at 7 and 14 days after ligation was signifi-
cantly increased (p < 0.05). Coadministration of gabapentin
with nortriptyline, at a 1: 1 ratio of their ED
50
, had a synergistic
effect, with an interaction index of 0.311 and 0.348 for these
mice at 7 and 14 days, respectively. Conclusion: The data
Received: September 26, 2014
Accepted after revision: December 1, 2014
Published online: January 15, 2015
Hugo F. Miranda
Pharmacology Program, School of Medicine
ICBM, Faculty of Medicine, Universidad de Chile
Independencia 1027, Santiago (Chile)
E-Mail hmiranda @ med.uchile.cl
© 2015 S. Karger AG, Basel
0031–7012/15/0952–0059$39.50/0
www.karger.com/pha
All authors contributed equally to this study.
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